1-(Oxan-4-yl)piperazine → (S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-4-[4-(6-hydroxy-2-oxo-1,4-dihydro-2H-quinazolin-3-yl)-piperidin-1-yl]-1-[4-(tetrahydropyran-4-yl)-piperazin-1-yl]-butane-1,4-dione

HRID 491162Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 491162
[NH2:1][C:2]1[C:33]([C:34]([F:37])([F:36])[F:35])=[CH:32][C:5]([CH2:6][C@@H:7]([CH2:11][C:12]([N:14]2[CH2:19][CH2:18][CH:17]([N:20]3[CH2:29][C:28]4[C:23](=[CH:24][CH:25]=[C:26]([OH:30])[CH:27]=4)[NH:22][C:21]3=[O:31])[CH2:16][CH2:15]2)=[O:13])[C:8](O)=[O:9])=[CH:4][C:3]=1[Cl:38].[O:39]1[CH2:44][CH2:43][CH:42]([N:45]2[CH2:50][CH2:49][NH:48][CH2:47][CH2:46]2)[CH2:41][CH2:40]1>>[NH2:1][C:2]1[C:33]([C:34]([F:37])([F:36])[F:35])=[CH:32][C:5]([CH2:6][C@@H:7]([CH2:11][C:12]([N:14]2[CH2:19][CH2:18][CH:17]([N:20]3[CH2:29][C:28]4[C:23](=[CH:24][CH:25]=[C:26]([OH:30])[CH:27]=4)[NH:22][C:21]3=[O:31])[CH2:16][CH2:15]2)=[O:13])[C:8]([N:48]2[CH2:47][CH2:46][N:45]([CH:42]3[CH2:43][CH2:44][O:39][CH2:40][CH2:41]3)[CH2:50][CH2:49]2)=[O:9])=[CH:4][C:3]=1[Cl:38]

Komponenten

3

Edukt 2

HCID 219423151-(Oxan-4-yl)piperazineHCID 68676153(S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-4-[4-(6-hydroxy-2-oxo-1,4-dihydro-2H-quinazolin-3-yl)-piperidin-1-yl]-4-oxo-butanoic acid

Produkt 1

HCID 57674019(S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-4-[4-(6-hydroxy-2-oxo-1,4-dihydro-2H-quinazolin-3-yl)-piperidin-1-yl]-1-[4-(tetrahydropyran-4-yl)-piperazin-1-yl]-butane-1,4-dione

Versuchsvorschrift

Prepared analogously to Example 81 from 80.0 mg (0.14 mmol) (S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-4-[4-(6-hydroxy-2-oxo-1,4-dihydro-2H-quinazolin-3-yl)-piperidin-1-yl]-4-oxo-butanoic acid and 24.5 mg (0.14 mmol) 1-(tetrahydropyran-4-yl)-piperazine.

Quellen und Nachweise

ORD-Eintrag
ord-af55537840354304926fb2cbda654202
Quelldatensatz
uspto-grants-2009_05
Patentnummer
US07528129B2

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